Microwave Assisted and Al2O3/K2CO3 Catalyzed Synthesis of Azetidin-2-One Derivatives Containing Aryl Sulfonate Moiety with Anti-Inflammatory and Anti-Microbial Activity

We report the novel synthesis of azetidin-2-one derivatives containing aryl sulfonate moiety from the reaction of 2-hydroxy benzaldehyde with p-toluene sulfonyl chloride afforded firstly 2-formylphenyl 4-methylbenzene sulfonate (2). The compound (2) on reaction with p-aminobenzoic acid or 2-aminopyridine gave the corresponding aldimines (3). Furthermore, the aldimines are on reaction with chloroacetyl chloride gives corresponding azetidin-2-ones in good to moderate yield. Among the eight synthesized azetidin-2-ones, five selected compounds have been screened for the an-ti-inflammatory activity, few of them showed good anti-inflammatory activity compared with standard drugs. Anti- microbial activity of all synthesized compounds has been tested and most of the compounds showed good anti-bacterial and anti-fungal activities.

3-Arylisothiazoloquinols as potent ligands for the benzodiazepine site of GABA_(A) receptors

3-Arylisothiazolo[5,4-b]quinolin-4(9H)-ones and 3-arylisoxazolo[5,4-b]quinolin-4(9H)-ones were synthesized and assayed for affinity for the benzodiazepine binding site of the GABAA receptors. While the 3-arylisothiazoloquinolin-4-ones were found to be potent ligands, with affinities (expressed as the affinity Ki value) down to 1 nM, the 3-arylisoxazoloquinolin-4-ones are less potent. This is suggested to depend on sterical repulsive interaction of the 3-arylisoxazoloquinolin-4-ones with the receptor essential volume of the binding site, and a higher electron density at the nitrogen in the azole ring (N-2) as well as the carbonyl oxygen in the isothiazoloquinolin-4-ones enabling them to interact stronger with hydrogen bond donor sites at the binding site.

Solvent-Free Mechanochemical Deprotection of N-Boc Group

Boc protection group could be readily removed in a very mild mechanochemical conditions. In a short reaction time, ball milling of Boc-protected amines with p-toluenesulfonic acid in solvent-free conditions affords corresponding amine p-TsOH salts.

Copper Salt of 12-Tungstophosphoric Acid： An Efficient and Reusable Heteropoly Acid for the Click Chemistry

烷基溴化物，钠叠氮化物和炔属羟联合的三个部件在 DMF 面对 triethyl 胺用交换铜的 phosphotungstic 酸(Cu-TPA ) 的催化数量被完成了与高选择在好收益负担得起代替的 triazoles。有趣地，与炔属羟联合烷基叠氮化物在房间温度乐意地继续在优秀收益供应 1,2,3-triazoles。催化剂能与活动的最小的减少为三～四随后的跑被恢复并且再使用。铜的使用修改了 heteropolyacids 使这个过程简单、方便、环境地友好。

Synthetic studies on the construction of 7-O-methylquercetin through regioselective protection and alkylation of quercetin

在从在在四个步骤的36%产量的橡黄素的 7-O-methylquercetin 的构造的合成研究被报导，在另一方面，这策略作为溶剂用 dephenyl 醚与 dichlorodiphenylmethane 一方面依靠儿茶酚组的选择保护在有本甲基溴化物的3氢氧根组的选择保护上，这二个不同保护组能在一样的加氢下面被移开。

Enantioselective construction of a congested quaternary stereogenic center in isoindolinones bearing three aryl groups via an organocatalytic formal Betti reaction

An efficient enantioselective formal Betti reaction between phenols and diaryl ketimines generated in situ from isoindolinone alcohols is described.In a reaction catalyzed by a chiral phosphoric acid,a broad range of ketimines and phenols afforded isoindolinone derivatives comprising a congested quaternary stereogenic center bearing three aryl groups in high yields,and high regioselectivities and enantioselectivities.